Arylguanidine and arylbiguanide binding at 5-HT3 serotonin receptors:: A QSAR study

For a series of monosubstituted arylguanidines, 5-HT3 receptor affinity was found generally related to the electron withdrawing nature of the substituent at the aryl 3-position and the lipophilicity of the 4-position substituent. A broader examination of 35 arylguanidines and arylbiguanides revealed that affinity could be described by molecular polarizability, a Chi index term ((8)chi(P)), and the sum of all (-Cl) E-State values (SsCl) in the molecule. (C) 2003 Elsevier Ltd. All rights reserved.